产品描述:
PD 198306 is an orally bioavailable and potent inhibitor of MAPK kinase 1/2 (MEK1/2; IC50 = 8 nM).{38577} It is selective for MEK1/2 over ERK, c-Src, PI3Kγ, and cyclin-dependent kinases (IC50s = >1 μM). PD 198306 (3-100 μM) reduces ERK1/2 phosphorylation and inhibits growth of HL-60 cells in vitro.{38578} In vivo, PD 198306 (10-30 mg/kg) reduces ERK1/2 phosphorylation and matrix metalloproteinase-1 (MMP-1) expression in a dose-dependent manner in a rabbit model of osteoarthritis.{38577} It also reduces ERK1/2 activity in the lumbar spinal cord and blocks static allodynia in rat models of neuropathic pain induced by streptozotocin (Item No. 13104) or chronic constriction injury.{38579}